中文名 | LGK974 |
英文名 | LGK974 |
别名 | NOVARTIS诺华 7'-二氯荧光素二乙酸酯 PORCUPINE抑制剂(LGK974) 2',3-二甲基-N-[5-(2-吡嗪基)-2-吡啶基]-[2,4'-联吡啶]-5-乙酰胺 2-(2,3-二甲基-[2,4-联吡啶]-5-基)-N-(5-(吡嗪-2-基)吡啶-2-基)醋胺石 |
英文别名 | LGK974 LGK-974 CS-1102 LGK-974 MK-0991, L-743872 LGK974(NVP-LGK974) 2',3-Dimethyl-N-[5-(2-pyrazinyl)-2-pyridinyl]-[2,4'-bipyridine]-5-acetamide 2-(2',3-Dimethyl-2,4'-bipyridin-5-yl)-N-[5-(2-pyrazinyl)-2-pyridi nyl]acetamide 2-(2',3-diMethyl-[2,4'-bipyridin]-5-yl)-N-(5-(pyrazin-2-yl)pyridin-2-yl)acetaMide 2-[5-Methyl-6-(2-methyl-4-pyridyl)-3-pyridyl]-N-(5-pyrazin-2-yl-2-pyridyl)acetamide |
CAS | 1243244-14-5 |
化学式 | C23H20N6O |
分子量 | 396.44 |
密度 | 1.268±0.06 g/cm3(Predicted) |
熔点 | 176 - 180°C |
沸点 | 650.9±55.0 °C(Predicted) |
溶解度 | 氯仿 (微溶) 、甲醇 (微溶) |
酸度系数 | 12.24±0.70(Predicted) |
存储条件 | Refrigerator |
外观 | 固体 |
颜色 | White to Off-White |
体外研究 | LGK-974在PORCN放射配体结合测定中,可有效取代[ LGK974能特异性地抑制三种RNF43突变细胞株HPAF-II, PaTu 8988S, 和 Capan-2的生长。 |
体内研究 | LGK-974 (3 mg/kg)作用于小鼠MMTV-WNT1肿瘤模型和人的头部和颈部鳞状细胞癌模型(hn30),抑制 Wnt 信号通路,诱导肿瘤退化且小鼠体重没有明显的下降。 LGK-974 (5 mg/kg, p.o., BID) 也能抑制RNF43-突变胰腺肿瘤(HPAF-II 和Capan-2)的生长。 |
参考资料 展开查看 | 1: Liu J, Pan S, Hsieh MH, Ng N, Sun F, Wang T, Kasibhatla S, Schuller AG, Li AG, Cheng D, Li J, Tompkins C, Pferdekamper A, Steffy A, Cheng J, Kowal C, Phung V, Guo G, Wang Y, Graham MP, Flynn S, Brenner JC, Li C, Villarroel MC, Schultz PG, Wu X, McNamara P, Sellers WR, Petruzzelli L, Boral AL, Seidel HM, McLaughlin ME, Che J, Carey TE, Vanasse G, Harris JL. Targeting Wnt-driven cancer through the inhibition of Porcupine by LGK974. Proc Natl Acad Sci U S A. 2013 Dec 10;110(50):20224-9. doi: 10.1073/pnas.1314239110. Epub 2013 Nov 25. PubMed PMID: 24277854; PubMed Central PMCID: PMC3864356. 2: Jiang X, Hao HX, Growney JD, Woolfenden S, Bottiglio C, Ng N, Lu B, Hsieh MH, Bagdasarian L, Meyer R, Smith TR, Avello M, Charlat O, Xie Y, Porter JA, Pan S, Liu J, McLaughlin ME, Cong F. Inactivating mutations of RNF43 confer Wnt dependency in pancreatic ductal adenocarcinoma. Proc Natl Acad Sci U S A. 2013 Jul 30;110(31):12649-54. doi: 10.1073/pnas.1307218110. Epub 2013 Jul 11. PubMed PMID: 23847203; PubMed Central PMCID: PMC3732970. |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 2.522 ml | 12.612 ml | 25.224 ml |
5 mM | 0.504 ml | 2.522 ml | 5.045 ml |
10 mM | 0.252 ml | 1.261 ml | 2.522 ml |
5 mM | 0.05 ml | 0.252 ml | 0.504 ml |
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